Alginate raft as carrier for self-emulsifying drug delivery system of curcuminoid: In vitro and in vivo analysis

Abstract

Hemorrhagic gastric ulcer can cause chronic inflammation that can lead to gastro-intestinal perforation and gastric adenocarcinoma or other serious gastric complications. Among naturally occurring treatments, curcumin (CuR) was used but it has limitations of low solubility and rapid first pass effect due to presence of diketo moiety. The present study aimed, to synthesize new synthetic derivative of CuR named curcuminoid (CuRD) and evaluate for its biological activity against gastric ulcer. Solubility and permeation of CuRD were enhanced by development of self-emulsifying drug delivery system (SEDDS). Pseudo-ternary phase diagram was constructed to identify the most efficient self-emulsification region. Optimized CuRD-SEDDS were further employed in the preparation of R-CuRD-SEDDS for local drug delivery in the stomach and all quality control test, raft resilience and strength, raft weight and volume, in-vitro dissolution, anti-oxidant and in-vitro anti-inflammatory activity were also observed. R-CuRD-SEDDS possess significant 20-fold increase in anti-oxidant and 10-fold increase in anti-inflammatory activities as compared to naturally occurring CuR. 70–80 % release within 1 hr, 85 % ulcer inhibition and 3.02 ± 1.5 ulcer index in aspirin induced ulcer was found. Newly developed R-CuRD-SEDDS with enhanced anti-oxidant and anti-inflammatory activities was an alternative approach for the treatment of gastric ulcer.